Chemistry of carbon compounds – Miscellaneous organic carbon compounds – C-metal
Patent
1976-10-08
1978-01-10
Coughlan, Jr., Paul M.
Chemistry of carbon compounds
Miscellaneous organic carbon compounds
C-metal
260250BC, 260518R, 424250, C07D24104
Patent
active
040678679
ABSTRACT:
There is disclosed a process for the preparation of the pyrazine precursor of methotrexate or an N-substituted derivative thereof and/or a di(lower)alkyl ester thereof having the formula: ##STR1## wherein R and R' may each be hydrogen or a lower alkyl group, e.g., ethyl. In a preferred embodiment, the process comprises reacting in one step the compounds aminomalononitrile, .beta.-halopyruvaldoxime and a di(lower)alkyl p-methylaminobenzoyl-L-glutamate to form the di(lower)alkyl ester of the pyrazine oxide precursor of methotrexate having the formula: ##STR2## This compound is then treated with either titanium trichloride oriodoformamidinium iodide to deoxygenate the compound. There is also disclosed a process for the preparation of a di(lower)alkyl ester of methotrexate having the formula: ##STR3## by treating the di(lower)alkyl ester of the pyrazine precursor of methotrexate with a guanidine salt of a weak organic acid, e.g., guanidine acetate.
REFERENCES:
patent: 2949466 (1960-08-01), Hoefle et al.
patent: 3134778 (1964-05-01), Weinstock et al.
Coughlan, Jr. Paul M.
Tovar Jose
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